IP Library › Granted Patent US 12,201,668
Granted Patent B2
US 12,201,668 · App. 16/662,932 · Granted Jan 21, 2025

Adiponectin peptidomimetics formulations

Inventors: Shikha P Barman (Bedford, MA); Kevin L Ward (Arlington, MA); Yugang Chen (Winchester, MA)
Assignee: Allysta Pharmaceuticals, Inc.
A61K38/10A61K47/10A61P27/02
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Quick Facts
Patent No.
US 12,201,668
App. No.
16/662,932
Granted
Jan 21, 2025
Kind
B2
Abstract

Disclosed are compositions and methods for the use of adiponectin peptidomimetics in therapeutic applications. The compositions can include a peptide, for example, D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , a solubilizer, a surfactant(s), a buffer, optionally boric acid and optionally mannitol. The osmolality of the composition can be between 260 to 330 mOsm/kg and the pH can be between 4.5 to 5.5. Methods of using the compositions in treating certain eye disease(s) are also disclosed.

Claims (29)

1. A composition comprising: a therapeutically effective amount of an adiponectin peptidomimetic having the formula of D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , a generally recognized as safe solubilizer, one or more generally recognized as safe surfactants, a buffer comprising boric acid and mannitol; wherein the osmolality is between 260 to 330 mOsm/kg and the pH is between 4.5 to 5.5.

2. The composition of claim 1 , wherein the solubilizer is selected from polypropylene glycol, glycerol, PEG400 and propylene glycol, the surfactant is selected from Polysorbate 80, Tyloxapol, Poloxamer, PEG 40 Hydrogenated Caster Oil, PEG 35 Caster Oil and PEG 40 Sterate, wherein the buffer further comprises an acetate buffer.

3. The composition of claim 2 , comprising, by weight: 0.01% to 2% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1% to 2% propylene glycol, 0.08% to 0.12% Tyloxapol or Poloxamer, 0.02% to 0.20% acetic acid and 0.05% to 0.5% sodium acetate.

4. The composition of claim 3 , comprising, by weight: 0.20% to 1.0% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.20% to 1.90% propylene glycol, 0.10% Tyloxapol or Poloxamer, 0.04% to 0.20% acetic acid and 0.08% to 0.42% sodium acetate.

5. The composition of claim 4 , selected from a composition comprising:

1.00% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.77% propylene glycol, 0.10% Tyloxapol, 0.14% acetic acid and 0.08% sodium acetate;

0.5% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.58% propylene glycol, 0.10% Tyloxapol, 0.09% acetic acid and 0.24% sodium acetate;

1.00% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.57% propylene glycol, 0.10% Tyloxapol, 0.09% acetic acid and 0.24% sodium acetate;

0.5% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.43% propylene glycol, 0.10% Tyloxapol, 0.04% acetic acid and 0.34% sodium acetate;

0.5% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.44% propylene glycol, 0.10% Tyloxapol, 0.04% acetic acid and 0.34% sodium acetate;

1.00% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.72% propylene glycol, 0.10% Poloxamer 188, 0.11% acetic acid and 0.09% sodium acetate;

0.51% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.73% propylene glycol, 0.10% Poloxamer 188, 0.11% acetic acid and 0.09% sodium acetate;

0.25% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.74% propylene glycol, 0.10% Poloxamer 188, 0.11% acetic acid and 0.09% sodium acetate;

0.50% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.55% propylene glycol, 0.10% Poloxamer 188, 0.10% acetic acid and 0.24% sodium acetate;

1.00% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.55% propylene glycol, 0.10% Poloxamer 188, 0.10% acetic acid and 0.24% sodium acetate;

1.00% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.40% propylene glycol, 0.20% Poloxamer 188, 0.19% acetic acid and 0.30% sodium acetate;

1.00% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.38% propylene glycol, 0.10% Tyloxapol, 0.19% acetic acid and 0.30% sodium acetate;

1.00% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.25% propylene glycol, 0.10% Tyloxapol, 0.17% acetic acid and 0.41% sodium acetate;

1.00% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.54% propylene glycol, 0.10% Tyloxapol, 0.19% acetic acid and 0.14% sodium acetate;

0.80% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.54% propylene glycol, 0.10% Tyloxapol, 0.19% acetic acid and 0.14% sodium acetate;

0.50% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.55% propylene glycol, 0.10% Tyloxapol, 0.19% acetic acid and 0.14% sodium acetate;

1.00% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.53% propylene glycol, 0.10% Tyloxapol, 0.19% acetic acid and 0.14% sodium acetate;

1.00% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.86% propylene glycol, 0.10% Tyloxapol, 0.13% acetic acid and 0.10% sodium acetate;

1.00% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.67% propylene glycol, 0.10% Tyloxapol, 0.15% acetic acid and 0.11% sodium acetate; and

1.00% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 1.62% propylene glycol, 0.10% Tyloxapol, 0.17% acetic acid and 0.13% sodium acetate.

6. The composition of claim 2 , comprising, by weight: 1.00% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 0.20% propylene glycol, 0.10% Tyloxapol, 0.07% acetic acid, 0.06% sodium acetate, 0.09% boric acid and 3.66% mannitol.

7. The composition of claim 2 , comprising, by weight: 0.401% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 0.193% propylene glycol, 0.097% Tyloxapol, 0.014% acetic acid, 0.138% sodium acetate, 0.09% boric acid and 3.65% mannitol.

8. The composition of claim 2 , comprising, by weight: 0.4% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 0.193% propylene glycol, 0.097% Tyloxapol, 0.015% acetic acid, 0.228% sodium acetate, 0.09% boric acid and 3.53% mannitol.

9. The composition of claim 2 , comprising, by weight: 0.1% D-Asn-Ile-Pro-Nva-Leu-Tyr-D-Ser-Phe-Ala-D-Ser-NH 2 , 0.193% propylene glycol, 0.097% Tyloxapol, 0.0065% acetic acid, 0.25% sodium acetate, 0.09% boric acid and 3.6% mannitol.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 13, 2021
From: BARMAN, SHIKHA P; WARD, KEVIN L; CHEN, YUGANG
To: ALLYSTA PHARMACEUTICALS, INC.
Reel/Frame 055908/0518 →
Continuity (2)
Provisional Application 62749861 · Oct 24, 2018
Related Publication 20200129585A1 · Apr 30, 2020
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